10results about How to "Reduce systemic side effects" patented technology

The invention discloses an ROS-responsive prostate cancer targeting prodrug as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The prodrug is formed by covalently linking a prostate cancer targeting peptide SYEELR, a ROS (reactive oxygen species) response type ketal thiol (TK) connexon and an active molecule Devimistat. The preparation method comprises the following two steps: firstly, coupling Devimistat with a TK linker to obtain an intermediate Dev-TK, and then coupling the intermediate Dev-TK with an SYEELR peptide fragment to obtain a target product. The prodrug can specifically break and release Devimistat in a tumor high active oxygen microenvironment, and active targeting delivery is realized by virtue of the SYEELR peptide. The invention provides a novel prostatic cancer treatment strategy with accurate targeting, controllable release, enhanced curative effect and toxicity reduction potential.

The present application relates to the technical field of medical apparatus, particularly relates to wearable and vibration control nail base nanocrystal microneedle transdermal drug delivery device, including shell, both sides of the shell are provided with a group of positioning notches respectively, a group of positioning notches are provided with a threaded hole respectively, the inside four corners of the shell are provided with a group of support seats respectively, still include controller assembly, nanocrystal microneedle assembly, vibration assembly, power supply assembly and fixed ring assembly, the controller assembly is detachably installed in the shell, the shell is provided with vibration assembly and battery assembly respectively, the bottom end of the shell is detachably provided with nanocrystal microneedle assembly, the both ends of the fixed ring assembly are detachably connected with a group of positioning notches respectively, the nanocrystal microneedle assembly is used for lightly pricking nail base epidermis and nail plate edge to form microchannel, the power supply assembly provides power for vibration assembly and controller assembly;It makes drug directly contact focus.

This invention discloses a compound preparation for treating vascular dementia and its preparation method. The active pharmaceutical ingredient consists of protopanaxadiol and gallic acid in a 1:1 mass ratio, and the dosage form is liposomes. The preparation method includes extraction, mixing, liposome preparation, and optional freeze-drying steps: protopanaxadiol and gallic acid are extracted and purified from ginseng rhizome and Terminalia chebula fruit, respectively. After mixing, they are combined with phospholipids and cholesterol to prepare a lipid membrane. The membrane is then homogenized by hydration, low-temperature ultrasound, and high-pressure microfluidic jet to obtain a homogeneous liposome suspension, which can be further freeze-dried into a freeze-dried powder. The 1:1 composition of protopanaxadiol and gallic acid targets multiple points on the pathological mechanism of vascular dementia, showing significant therapeutic effects and broad application prospects. This preparation uses a liposome dosage form to improve the bioavailability of the active ingredient, the preparation process parameters are controllable, the active ingredient has high purity, the liposomes have uniform particle size, high encapsulation efficiency, and good stability.

The invention discloses a brain-targeted nasal-spray amphotericin B phospholipid complex and a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations, the brain-targeted nasal-spray amphotericin B phospholipid complex is prepared by adopting a film dispersion method, and the preparation method comprises the following steps: dissolving 15-hydroxystearic acid polyethylene glycol ester, phospholipid, cholesterol, amphotericin B and optional other auxiliary components in a solvent, removing the solvent until a film is formed, and drying to obtain the brain-targeted nasal-spray amphotericin B phospholipid complex. And carrying out hydration dispersion to obtain the amphotericin B-loaded phospholipid complex. According to the amphotericin B sodium deoxycholate injection, the problems that the traditional amphotericin B sodium deoxycholate injection is high in renal toxicity, the intrathecal injection is poor in solubility, and low in bioavailability and patient compliance, large in side effect and the like due to the fact that the traditional amphotericin B sodium deoxycholate injection is difficult to penetrate through a blood brain After nasal administration, the drug is quickly delivered into the brain, so that the slow release of the drug is realized, the intracerebral bioavailability of the drug is improved, high brain targeting and low systemic toxic and side effects are realized, and good clinical application value and market prospect are achieved.

This invention discloses a nystatin microsphere with targeted enhanced antifungal function, its preparation method, and its application. The microsphere uses sodium alginate as a carrier, internally encapsulating the antifungal drug nystatin. The surface is covalently modified with the β-glucan binding domain of the Dectin-1 protein, constructing a smart drug delivery system with fungal targeting function. The microsphere preparation process is simple and reproducible, and can be scalable using an emulsion-ionic crosslinking method combined with protein coupling technology. In vitro characterization shows that the microspheres have uniform particle size and stable dispersion, and Dectin-1 modification significantly enhances their specific binding ability against Candida albicans. This targeted delivery system, while successfully preserving drug activity, significantly improves the antifungal efficiency of nystatin through Dectin-1-mediated targeting, achieving efficacy close to that of free drug, and providing a new strategy for constructing highly efficient and long-acting antifungal agents.

This invention discloses a targeted, temperature-sensitive drug-loaded composite microsphere based on attapulgite, comprising primary drug-loaded composite microspheres and lauric acid. The primary drug-loaded composite microspheres include purified attapulgite, gypenosides, inulin, and folic acid. Gynostemma pentaphyllum saponins, inulin, and folic acid are adsorbed onto a mesoporous structure composed of purified attapulgite rod crystals. The surface rigid structure of the primary drug-loaded composite microspheres includes a large number of interlaced channels. Lauric acid is encapsulated within the surface rigid structure of the primary drug-loaded composite microspheres. The mass percentages of purified attapulgite, gypenosides, inulin, and folic acid are: 50-85 parts: 10-30 parts: 10-25 parts: 0.1-1 parts; the mass ratio of the primary drug-loaded composite microspheres to lauric acid is 1:2 to 1:3. This application not only enables temperature-controlled "on-off" drug release, significantly improving drug targeting and therapeutic precision, but also reduces the systemic toxicity of chemotherapy at its source, achieving highly efficient and low-toxicity synergistic therapy.

The invention discloses an ultrasonic labeling guided targeting nano liquid drop. The nano liquid drop comprises an inner core and a polymer layer coating the surface of the inner core, the inner core is perfluorinated carbon; the polymer layer comprises fluorine-containing polycaprolactone, a copolymer as shown in a formula I, an ultrasonic activation prodrug and a sound-sensitive agent; the perfluorinated carbon can be dissolved by the fluorine-containing polycaprolactone. According to the application, the tumor tissue is precisely treated by utilizing ultrasound to induce the tumor tissue to highly express the heat shock protein, so that the nano liquid drops modified with the heat shock protein targeting polypeptide are efficiently enriched at the tumor part, and the difference between the drug concentration in the tumor tissue and the drug concentration in other normal tissues is remarkably increased; the drug targeting selectivity and the drug release accuracy are improved.

This invention discloses a sonodynamic synergistic thrombolysis system and its application. The system includes a tissue plasminogen activator variant, a sonosensitive agent, and an ultrasound source. The tissue plasminogen activator variant is an intravenously administered formulation, the sonosensitive agent is an intravenously infused formulation, and the ultrasound source is used to emit ultrasound during sonosensitive agent administration to activate the agent. This invention significantly improves thrombolysis efficiency and reduces thrombolytic agent dosage and bleeding risk through the dual synergistic effect of TNK-tPA enzymatic hydrolysis and sonodynamic chemical oxidation. The system can significantly improve vascular recanalization rate and blood flow velocity recovery rate, and has high biocompatibility. This invention is applicable to thrombolytic treatment of various thrombotic diseases and has the advantages of simple operation, strong targeting, and wide application range.

The invention discloses a parabacteroides coumarini vesicle nano preparation for PD-L1 targeted synergistic chemotherapy as well as preparation and application of the parabacteroides coumarini vesicle nano preparation. The nano preparation takes a parabacteroides coumarini-sourced membrane vesicle as a carrier, a chemical drug apatinib is loaded in the nano preparation, the surface of the nano preparation is modified with an anti-PD-L1 antibody through chemical coupling, and the nano preparation is named as Apatinib-MVsaPD-L1; according to the nano preparation, apatinib and a PD-L1 antibody can be synergistically delivered to a breast cancer focus, so that the synergistic interaction of chemotherapy and immune checkpoint blocking is realized; in-vitro experiments show that the nano preparation can significantly inhibit proliferation of breast cancer cells and induce apoptosis of the breast cancer cells; in-vivo experiments show that the compound can effectively inhibit tumor growth and remarkably increase infiltration of CD8 < + > T cells and TNF-alpha < + > CD8 < + > T cells in a tumor microenvironment, has no toxic or side effect, and provides a new safe and efficient drug delivery platform for combined treatment of breast cancer.

This invention relates to the field of biopharmaceutical technology, and in particular to an antibody-targeted modified dual-strain prebiotic delivery system, its preparation method, and its applications. This invention modifies VCAM-1 antibody fragments onto *AKK* bacteria and *Bifidobacterium lactis* Probio-M8, then utilizes fructooligosaccharides and inulin as prebiotics to enhance probiotic metabolism and promote intestinal colonization. Finally, it coats the system with hydroxypropyl methylcellulose phthalate (HPMCP) enteric coating to construct the antibody-targeted modified dual-strain prebiotic delivery system—V-PM8-Am-FI-HPMC. The V-PM8-Am-FI-HPMC provided by this invention can simultaneously achieve intestinal flora regulation, lipid metabolism balance, inflammation suppression, ischemia improvement, and vascular anti-calcification, ultimately achieving the purpose of treating and / or improving atherosclerosis, while ensuring targeting and safety.